533062 S1P3 Receptor Antagonist, TY-52156 - Calbiochem

533062
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₈H₁₉Cl₂N₃O

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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable hydrazonamide derivative that acts as a selective and competitive antagonist of S1P3 receptor (Ki = 110 nM) and suppresses S1P-induced expansion of A549, LNCaP, U251MG, and OVCAR-5 cancer cells (~ 10 µM). Displays about 30-fold lower effect on S1P1, S1P2, S1P4, or S1P5 receptors and does not affect 24 different G-protein coupled receptors (~10 µM). Shown to block S1P-induced expression of Hes1 and reduce ALDH-positive cell population. Inhibits the tumorigenicity of SphK1-overexpressing ALDH-positive cells following chronic administration over a period of 6 weeks. Preferentially inhibits S1P-induced increase in [Ca2+]i and Rho activation in vascular smooth muscle cells. Shown to reduce S1P3 receptor-induced bradycardia in vivo in rats and diminishes coronary flow in perfused rat heart. Also shown to relax cerebral arteries precontracted with S1P.

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number533062
      Brand Family Calbiochem®
      SynonymsS1P3 Antagonist, TY-52156, Sphingosine 1-phosphate Receptor Antagonist, TY-52156, TY52156, TY 52156, [1-Chloro-1-(4-chlorophenylhydrazono)]-3,3-dimethyl-2-butanone
      DescriptionS1P3 Receptor Antagonist, TY-52156
      References
      ReferencesHirata, N., et al. 2014, Nat. Comm. 5, in press.
      Murakami, A., et al. 2010. Mol. Pharm. 77, 704.
      Product Information
      FormOrange solid
      Hill FormulaC₁₈H₁₉Cl₂N₃O
      Chemical formulaC₁₈H₁₉Cl₂N₃O
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetS1P3
      Purity≥98% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 4 weeks at -70°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      S1P3 Receptor Antagonist, TY-52156 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Hirata, N., et al. 2014, Nat. Comm. 5, in press.
      Murakami, A., et al. 2010. Mol. Pharm. 77, 704.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision09-September-2016 JSW
      SynonymsS1P3 Antagonist, TY-52156, Sphingosine 1-phosphate Receptor Antagonist, TY-52156, TY52156, TY 52156, [1-Chloro-1-(4-chlorophenylhydrazono)]-3,3-dimethyl-2-butanone
      DescriptionA hydrazonamide derivative that suppresses the S1P-induced cancer stem cell expansion effects in multiple human cancer cell lines including, breast cancer MCF-7 cells, lung cancer A549 cells, glioma U251MG cells and ovarian cancer OVCAR-5 cells at 10 µM. Significantly inhibits the tumorigenicity of SphK1-overexpressing ALDH-positive cells after chronic continuous injection for 6 weeks (167mg/ml) in a mouse xenograft model. In addition, shown to suppress the S1P-induced effects such as Ca2+ increase and Rho activation in vascular smooth muscle cells and decrease of coronary flow in isolated perfused rat hearts.
      FormOrange solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₈H₁₉Cl₂N₃O
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage -20°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 4 weeks at -70°C.
      Toxicity Standard Handling
      ReferencesHirata, N., et al. 2014, Nat. Comm. 5, in press.
      Murakami, A., et al. 2010. Mol. Pharm. 77, 704.